氨苄西林钠.pdf

氨苄西林钠氨苄西林钠别名：氨苄西林、氨苄青、安比西林、沙维西林、赛米西林、氨苄西、潘别丁、AB-PC。参考资料Ampicillin(Penbritin,BRL1341)【作用与用途】本品为广谱半合成青霉素，毒性极低。抗菌谱与青霉素相似，对青霉素敏感的细菌效力较低，对草绿色链球菌的抗菌作用与青霉素相仿或略强。对白喉杆菌、破伤风杆菌和放线菌其效能基本和青霉素相同。对肠球菌及李司忒菌的作用则优于苄青霉素。对耐药葡萄球菌及其它能产生青霉素酶的细菌均无抗菌作用。对革兰阴性菌有效，但易产生耐药性。本品主要用于敏感菌所致的泌尿系统、呼吸系统、胆道、肠道感染以及脑膜炎、心内膜炎等。主要用于伤寒、副伤寒的治疗；也用于泌尿道、呼吸道感染。【剂量与用法】口服，2g6g/日，分 34 次，空腹服用。儿童，每日 100mg/kg，分 34 次，空腹服用。肌注或静注，成人，2g4g/日；儿童，每日 50mg100mg/kg，一般每 46 小时1次。静注给药可分次徐缓静脉推注或静滴；静滴，1 次 1g2g，溶于100ml输液中，滴注1/21小时，24 次/日。儿童，每日 100mg150mg/kg，分次给予。【副作用】1 本品可致过敏性休克，皮疹发生率较青霉素为高。有时也发生药热。2 本品注射前必须做皮试，阴性者方可使用。有青霉素过敏史者禁用。通用名称：氨苄西林英文名称：Ampicillin中文别名：氨比西林、氨苄青、氨苄青霉素钠、安比西林、胺苄青霉素英文别名：Alpen、Amperil、Ampicillinum、Ampilan、Omnipen、Penbritin、Penbriton、Polycillin、Principen、Servicillin、Sodium Ampicillin【药理】药效学参阅青霉素。氨苄西林对革兰阳性球菌和杆菌(包括厌氧菌)的抗菌作用基本与青霉素相同，但对粪球菌的作用较后者为弱。革兰阴性细菌中脑膜炎球菌、淋球菌、流感杆菌、百日咳杆菌、布氏杆菌、变形杆菌、沙门菌等皆对本品敏感。多数大肠杆菌及某些志贺菌属也对本品敏感，但后者可迅速出现耐药性。氨苄西林对军团菌和胎儿弯曲杆菌有抗菌作用。除脆弱类杆菌外，其余厌氧革兰杆菌多对本品敏感。药动学肌内注射 0.5g 氨苄西林，0.5l 小时血药浓度达峰值，血药峰浓度为 12(714)g/ml；6 小时的血药浓度为 0.5g/ml。静脉注射 0.5g 后 15 分钟和 4 小时的血药浓度分别为 17 和 0.6g/ml。本品对胃酸相当稳定，因此口服后吸收良好，但受食物影。空腹口服lg，2小时血药浓度达峰值，为 7.6g/ml，6 小时的血药浓度为 1.1g/ml。1/2 为 1.5 小时。新生儿和早产儿按体重肌内注射 10mg/kg 和 25mg/kg 后 l 小时，血药浓度达峰值，分别为 20和 60g/ml，1/2 为 1.74 小时。孕妇血清中氨苄西林浓度明显较非妊娠期为低。氨苄西林的体内分布良好。细菌性脑膜炎病人每日按体重静脉注射 150mg/kg，前3 天脑脊液中浓度可达 2.9g/ml，以后浓度将随炎症减轻而降低。正常脑脊液中仅含少量氨苄西林。本品可透过胎盘到达胎儿循环，羊水中可有持续浓度。肺部感染病人的支气管分泌液中浓度为同期血药浓度的 l/50。胸腹水、关节腔积液、眼房水、乳汁中皆含相当量的本品。伤寒带菌者 B 管胆汁中浓度平均为血药浓度的 3倍多，最高可达17.8 倍。本品分布容积为 0.28L/kg。蛋白结合率为 2025。1250的本品在肝内代谢。氨苄西林的肾清除率较青霉素略缓，部分通过肾小球滤过，部分通过肾小管分泌。口服后 24 小时尿中排出的氨苄西林为给药量的 2060，肌内注射为 50,静脉注射为 70。少量(0.1)自胆汁中排泄。丙磺舒可使本品在肾的清除变缓。氨苄西林可为血液透析清除，但腹膜透析对本品的清除无影响。【适应症】用以治疗敏感细菌所致的呼吸道感染、胃肠道感染、尿路感染、软组织感染、脑膜炎、败血症、心内膜炎等。【用法用量】1成人肌注剂量为每日 24g，分4 次给予；静脉给药剂量每日 412g，分 24 次，每日最高剂量为 16g。2小儿肌注剂量为每日按体重 50100mgkg，分4 次；静脉给药剂量每日按体重 100200mgkg，分 24 次，每日最高剂量为按体重 300mgkg。3足月产新生儿按体重每次 12.550mg/kg，肌内注射或缓慢静脉推注；出生后前 48 小时每 12 小时一次；第 3 日2 周每 8 小时一次，以后每 6 小时一次。早产儿第一周、14 周和 4 周以上按体重每次 12.550mgkg，分别为每 12 小时、8 小时和 6 小时一次。4肾功能减退、晚期肾功能衰竭病人氨苄西林半衰期可自正常人的 1.5 小时延长至 720 小时，因此氨苄西林给药间期在肾小球滤过率(GFR)为 1015ml/min 和小于10ml/min 时应分别延长至 612 小时和 1216 小时。5口服成人每日 24g，分 4 次服用；小儿每日按体重 50100mgkg，分4 次服用。制剂与规格按氨苄西林计。氨苄西林钠胶囊(1)0.25g(2)0.5g注射用氨苄西林钠(1)0.5g(2)1g口服:一次0.25-1g 一日4次;肌肉注射:一日4-6g,分4次用;静脉滴注:一日 4-12g,分2-4 次用,儿童一日 100-150mg/kg,分次给予.【禁用慎用】青霉素过敏者忌用.【给药说明】参阅青霉素钠。晚期妊娠孕妇应用氨苄西林后可使血浆中结合的雌激素浓度减少，但对不结合的雌激素和孕激素无影响。【不良反应】本品的不良反应与青霉素钠相仿，以过敏反应较为多见。皮疹是最常见的反应，多发生于用药后 5 天，呈荨麻疹或斑丘疹，前者为青霉素过敏反应的典型皮疹，后者对氨苄西林有一定的特异性，注射给药的皮疹发生率高于口服者。传染性单核细胞增多症、巨细胞病毒感染、淋巴细胞白血病、淋巴瘤等病人应用本品时易发生皮疹，因此，本品不能用于这些病人。粒细胞和血小板减少偶见于应用氨苄西林的病人，氨苄西林相关肠炎也极为罕见。少数病人出现血清丙氨酸氨基转移酶升高。大剂量氨苄西林静脉给药可发生抽搐等神经系统毒性症状，婴儿应用氨苄西林后可出现颅内压增高，表现为囱隆起。极大量氨苄西林可能发生听力障碍，但氨苄西林的耳毒性尚未最后确定。氨苄西林所致的间质性肾炎亦有报告。氨节西林不良反应的防治与青霉素钠同。可引起皮疹,药热,寒战,面部潮红或苍白,气喘,呼吸困难,心悸,胸闷,紫绀,腹痛,过敏性休克等.口服后个例可出现恶心,呕吐和腹泻.少数患者可有白细胞减少.暂时性血清转氨酶升高,也可有急性腮腺肿大,全身散在出血点,肾功能异常.氨苄西林皮疹发生率为 3.118，常在开始治疗后 712 天出现，此为过敏反应所致。斑丘疹占整个皮疹的 2/3，单核细胞增多症的病人应用本药，斑丘疹、紫癜性皮疹的发生率为 42100，肾功能不全的病人皮疹发生率也较高。药疹的发生率与用药时间长短及剂量大小无关，而与感染病种、年龄及性别有一定关系。伤寒患者及革兰氏阴性杆菌败血症患者的药疹发生率最高；结缔组织病、白血病及肿瘤合并感染症者次之，肝胆及泌尿系感染者的药疹高于胃肠道及呼吸道感染者。在病毒性疾病、流行性出血热、脑炎及传染性单核细胞增多症患者的药疹发生率均明显较高。年龄 50岁以下者较 50 岁以上者药疹发生率明显增高(17.5对 5.4)(P0.01)，女性的发生率明显高于男性，分别为 16.8及 7.3(P0.01)。少数病人可出现肾病，此为免疫学反应，免疫复合物及补体成份可沉积于肾小球和血管中，导致肾小球肾炎。有报道：静推氨苄西林钠促使高血压病急剧恶化的病例。分析认为：氨苄西林易致过敏性间质性肾炎、肾素增高，导致继发性高血压。口服本品 1 周，约11病人发生腹泻。有 1/4 病人发生氨基转移酶升高。陈风云报道：8 名患者因其它感染性疾病而用氨苄西林静滴，用药后除均出现皮肤瘙痒及不同形状的皮疹外，并有不同程度的肝损害。其中原有肝炎的两例病人因病情加重而死亡。日本学者指出，药物变态反应性肝损害是由于药物对肝脏的直接损害，使肝细胞的部份细胞膜成分发生变化，游离的载体蛋白再与药物结合获得抗原性，从而引起变态反应性肝损害。尿路感染病人在治疗期间可出现变形杆菌、产气杆菌及白色念珠菌的二重感染。【相互作用】参阅青霉素钠。(1)氨苄西林与氯霉素联合应用后，在体外对流感杆菌的抗菌作用影响不一，氯霉素在高浓度(510g/ml)时对本品无拮抗现象，在低浓度(12g/ml)时可使氨苄西林的杀菌作用减弱，但对氯霉素的抗菌作用无影响。氨苄西林与氯霉素联合后在体外对 21 株脑膜炎球菌抗菌活性的影响如下；出现拮抗者 13 株、累加者 5 株，协同者 3 株。对 21 株肺炎球菌呈现拮抗作用者仅 1 株，累加作用者 14 株，协同现象者 6 株。氨苄西林在体外对金葡菌的抗菌作用可为林可霉素所抑制。氨苄西林对大肠杆菌、变形杆菌和肠杆菌属的体外抗菌作用可为卡那霉素所加强。庆大霉素可加速氨苄西林对 B 组链球菌的体外杀菌作用。氨苄西林或阿莫西林对产-内酰胺酶的淋球菌的最低抑菌浓度为 64g/ml，棒酸的联合应用可使这两种青霉素的最低抑菌浓度降至 4g/ml。(2)本品与下列药品有配伍禁忌：硫酸阿米卡星、卡那霉素、庆大霉素、链霉素、磷酸克林霉素、盐酸林可霉素、粘菌素甲磺酸钠、多粘菌素 B、琥珀氯霉素、红霉素乙基琥珀酸盐和乳糖酸盐、四环素类注射剂、新生霉素、肾上腺素、间羟胺、多巴胺、阿托品、盐酸肼酞嗪、水解蛋白、氯化钙、葡萄糖酸钙、维生素 B族、维生素 C、含有氨基酸的营养注射剂、多糖(如右旋糖酐 40)和氢化可的松琥珀酸钠，这些药物可使氨苄西林的活性丢失。(3)别嘌醇可使氨苄西林皮疹反应发生率增加，尤其多见于高尿酸血症。氯霉素和氨苄西林合用时，远期后遗症的发生率较两者单用时为高。(4)氨苄西林能刺激雌激素代谢或减少其肠肝循环，因而可降低口服避孕药的效果。【儿童用药】【老年患者用药】老年患者应根据肾功能情况调整用药剂量或用药间期。【注意事项】1.患者每次开始应用本品前，必须先进行青霉素皮试。2.对头孢菌素类药物过敏者及有哮喘、湿疹、枯草热、荨麻疹等过敏性疾病史者慎用。3.本品与其他青霉素类药物之间有交叉过敏性。若有过敏反应产生，则应立即停用本品，并采取相应措施。4.肾功能减退者应根据血浆肌酐清除率调整剂量或给药间期。5.对怀疑为伴梅毒损害之淋病患者，在使用本品前应进行暗视野检查，并至少在四个月内，每月接受血清试验一次。6.长期或大剂量应用本品者，应定期检查肝、肾、造血系统功能和检测血清钾或钠。7.对实验室检查指标的干扰：（1）硫酸铜法尿糖试验可呈假阳性，但葡萄糖酶试验法不受影响；（2）可使血清丙氨酸氨基转移酶或门冬氨酸氨基转移酶测定值升高。Benzyl ampicillin-resistant(ampicillin)Synonyms:ampicillin,benzyl ammonia Green,ampicillin,沙维西林,米西林 tournament,ammonia benzyl West,PanDo not Ding,AB-PC.References Ampicillin(Penbritin,BRL1341)Therole and use【】This product is broad-spectrum semi-synthetic penicillin,anextremely low toxicity.Antibacterial spectrum and penicillin are similar to penicillin-sensitive bacteriainthe lowereffectiveness of viridans streptococci with penicillin antimicrobial activity similar to orSlightly.Bacillus of diphtheria,tetanus bacilli and actinomycetes its basic and penicillin thesame performance.Of enterococci and listeria bacterias role is better than benzylpenicillin.Ofdrug-resistant Staphylococcus aureusand other productiveHealth penicillinase no antibacterial effect of bacteria.Gram-negative bacteria for effective,but easy to producedrug resistance.This product is mainly used for 敏感菌 induced urinary system,respiratory,biliary,intestinalinfections and meningitis,endocarditis,etc.Mainly used for typhoid,paratyphoid treatment;also used for urinary tract,respiratory tractinfection.【Usage】dose andOral,2g 6g/day divided into 3 4 times,anempty stomach.Children,daily 100mg/kg,at3 4 times,anempty stomach.Intramuscular or intravenous,adult,2g 4g/day;children,daily50mg 100mg/kg,generally every 4 6 hours one time.Intravenous administration can be dividedinto sub-slow intravenous injection or intravenous drip;infusion,1 1g 2g,dissolvedin100mlinfusion,theinfusion of 1/2 1 hour,2 4 times/day.Children,thedaily 100mg 150mg/kg,at times given.Side effects【】One product can Anaphylactic shock,rash incidence is higher than the penicillin.Sometimeshappen drug hot.Twogoods must be done before injection skin test,negative use only.History of penicillinallergy whohave disabled.Generic Name:ampicillinEnglish name:AmpicillinEnglish Synonyms:ammonia than resistant,ammonia benzyl Green,ampicillin sodium,ampicillin,benzylpenicillin amineEnglish Synonyms:Alpen,Amperil,Ampicillinum,Ampilan,Omnipen,Penbritin,Penbriton,Polycillin,Principen,Servicillin,Sodium Ampicillin【Pharmacological study】PharmacodynamicsSee penicillin.Ampicillin against Gram-positive cocci and bacilli(including anaerobes)Antibacterial effect of basic and penicillin the same,but therole of fecal bacteria than the latter fortheweak.Gram-negative bacteriaMedium meningococcal,gonococcal,influenza bacillus,Bordetella pertussis,Brucella,Proteus,Salmonella 菌等 are sensitive to thechemicals.Themajority of E.coli and some Shigellais also sensitive to thechemicals,But the latter can rapidly emerging drug resistance.Ampicillin against Legionella andCampylobacter fetus has antibacterial activity.Inaddition to Bacteroides fragilis,other anaerobicgram-bacilli sensitive to many of thegoods.Pharmacokinetics0.5g intramuscular injection of ampicillin,0.5 l-hour peak plasma concentration,peakplasma concentration of 12(7 14)g/ml;6-hour plasma concentration of 0.5g/ml.Afterintravenous injection of 0.5g15 minutes and 4 hours of blood drug concentrations were 17 and 0.6g/ml.This product isquite stableonthe gastric acid,so good oral absorption,but the impact of food.Fasting oral lg,2hoursplasma concentration TatsuPeak,inorder to 7.6g/ml,6-hour plasma concentration of 1.1g/ml.T1/2 for 1.5 hours.Newborn and premature infants by intramuscular injection of 10mg/kg body weight and 25mg/kgafterthe l-hour plasmaconcentrationDegrees,reached thepeak,respectively,20 and 60g/ml,T1/2 1.7 4 hours.Maternal serumconcentrations of ampicillin significantly lower than that of non-pregnancy.Good distribution ofampicillininvivo.Bacterial meningitisYansick a day according to the weight intravenous 150mg/kg,before three daysincerebrospinal fluid concentrations of up to 2.9g/ml,after the concentration will be lowered withthealleviation of inflammation.Only a small amount of cerebrospinal fluidinnormalampicillin.Product can reach the fetal circulation through the placenta,amniotic fluid may havesustained concentration.Patient lung infectioninthe bronchial secretion for the same period theconcentration of plasma concentration of l/50.Hydrothorax and ascites,joint effusion,Aqueous humor,breastmilk contains a considerable amount ofallthe goods.Typhoid carriers,the concentration of bile tube B average plasma concentration of 3 times up to 17.8 times.Thevolume of distribution forgoods0.28L/kg.ProteinCombined rate of 20 25%.12 50%of the goods at the liver metabolism.The renalclearance rate of ampicillin than penicillin ease slightly,inpart,through glomerular filtration,inpart through renal tubular secretion.Afteroral administration24-hour urine discharged from the dosage of ampicillin for 20 60%,50%forintramuscularinjection,intravenous injection of 70%.Asmall number(0.1%)from the bile excretion.Probenecidallows this goodsinrenalclearanceInaddition to slowing down.Ampicillin for hemodialysis clearance,but peritoneal dialysisclearanceof the goodshad no effect.【Indications】For the treatment of sensitive bacteria caused by respiratory infections,gastrointestinal tractinfections,urinary tract infection,soft tissueinfections,meningitis,septicemia,endocarditis,etc.【Usage consumption】1.Adult daily dose intramuscular injection of 2 4g,sub 4 sub-grant;intravenous dose daily4 12g,at 2 4 times the maximum daily dose of 16g.2.Intramuscular daily doseinchildren according to the weight 50 100mg/kg,at 4 times;intravenous daily dose according to theweight 100 200mg/kg,at 2 4 times the maximum dailydose according to theweight300mg/kg.3.Full-term newborns according to the weight of each 12.5 50mg/kg,intramuscularinjectionorslow intravenous injection;48 hours after birth beforethe 12 hours each time;the firstday 3 8 hoursevery two weeksonce,inordertoEvery 6 hours.The first week of prematurity,1 4 weeks and 4 weeks according to theweight of each 12.5 50mg/kg,respectively,foreach 12 hours,8 hoursand 6 hours.4.Renal dysfunction,advanced renal failure patients from normal ampicillin half-life can beextended to 1.5 hours of 7 to 20 hours,so between the administration of ampicillinintheglomerular filtration rate(GFR)for less than 10 15ml/min and 10ml/min,respectively,should be extended to 12hoursand 6 12 16 hours.5.Adult daily oral 2 4g,sub 4 sub-taking;children daily according to the weight 50 100mg/kg,sub 4 sub-taking.Preparation and specifications by ampicillin dollars.Ampicillin Sodium Capsule(1)0.25g(2)0.5gAmpicillin Sodium Injection(1)0.5g(2)1gOral:0.25-1g a day 4 times;intramuscular injection:day 4-6g,at 4 times;intravenous drip:day 4-12g,at 2-4 times,childrens day 100-150mg/kg,sub-sub-grant.Used with caution】【Prohibited忌用 penicillin allergy.【Description】deliverySee penicillin sodium.Pregnant womeninlate pregnancy,after theapplication of ampicillininplasma can combine to reduce the concentration of estrogen,but not combined estrogen andprogesterone had no effect.Adverse reactions【】This product adverse reaction with sodium penicillin similar to allergic reactions more often.Rash is themost common response,many occurredin5 days after administration,wereurticariaorrash,theformer forthe penicillinThetypical allergic reaction skin rash,which has a certain degree of specificity of Ampicillin,injection drug rash incidence werehigher than the oral.Infectious mononucleosis,cytomegalovirusinfection,lymphaticLeukemia,lymphoma patients should be prone to occur when 用本品 rash,therefore,thegoods can not be used for these patients.Neutrophil and platelet reductioninthe application ofampicillin occasional patients,ammonia benzylWestLin-related enteritis also extremely rare.Asmall number of patients the serum alanineaminotransferase increased.High-dose intravenous administration of ampicillin convulsions canoccur,suchasnervous system toxicity symptoms,theapplication of ammonia benzyl babyAfter the emergence of resistant intracranial hypertension can be demonstrated for thechimney uplift.Ampicillin probably happen very substantial hearing impairment,but ototoxicity ofampicillin has not yet been finalized.Ampicillin-induced interstitialrenalYanalso report.Ammonia resistant section of the prevention and treatment of adverse reactions with sodiumand penicillin.Can cause skin rashes,drug fever,chills,facial flushingorpallor,shortness of breath,dyspnea,palpitations,chesttightness,cyanosis,abdominal pain,suchasanaphylactic shock.个 patients afteroral administration may be nausea,vomiting and diarrhea.MinorityPatients may have leukopenia.Transient increaseof serum transaminase,may also have acuteparotid swelling,generalized sporadic bleeding,therenal dysfunction.The incidence of ampicillin rash was 3.1 18%,often beginning after treatment at 7 to 12days,this is caused byanallergic reaction.Rash rash total of 2/3,mononucleosis patients shouldbeUsing this medicine,rash,purpuricrash incidencewas 42 100%,renalinsufficiency patientshave ahigher incidence ofskinrash.The incidence of drug eruption and the length of time and dose-dependent reductionindruguse has nothing to do with the infection disease,age and sex relationship must have.Typhoidpatients and gram-negative bacilliinpatients with sepsishair drug eruptionThehighest rate;connective tissuedisease,leukemia and tumor disease werefollowed by co-infection,liver and gall-bladder and urinary tract infection drug eruption were higher than thegastrointestinal tract and respiratory tract infection.Inviral diseases,epidemic ofBlood hot,encephalitis and infectious mononucleosis patients with the incidence of drugeruption were significantly higher.Age under 50 years of age than those over the age of 50 theincidence of drug eruption weresignificantly increased(17.5%vs 5.4%)(P 0.01),the incidence of females was significantly higher than men,respectively 16.8%and7.3%(P 0.01).Asmall number of patients with kidney disease can occur,this study for immune response,immune complexes and complement components may be depositedinthe glomeruli and bloodvessels,resultinginglomerulonephritis.Ithas been reported:static pushing and promotingAmpicillin SodiumSo that the sharp deterioration of hypertension cases.Analysis:ampicillin 易致 allergicinterstitial nephritis,renin increased,resultinginsecondary hypertension.Oral administration ofthegoods one week,about 11%of diarrhea patients.Thereis 1/4 sick elevated aminotransferase happen.Chen Fengyun reported:eight patientswith other infectious diseases due to the use of intravenous ampicillin,both after administrationinaddition to itching and skin rashes of different shapes of thingsAnd have varying degrees of liver damage.One